公开(公告)号：US20100190789A1

公开(公告)日：2010-07-29

申请号：US12663013

申请日：2008-06-06

申请人： Jean-Pierre Andre Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J.M De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Peter Vladimirivich Davidenko

发明人： Jean-Pierre Andre Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J.M De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Peter Vladimirivich Davidenko

IPC分类号： A61K31/5377 ,  C07D241/04 ,  A61K31/495 ,  C07D401/12 ,  A61K31/496 ,  C07D403/10 ,  C07D405/12 ,  C07D403/12 ,  C07D413/12 ,  C07D211/34 ,  A61K31/451 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

CPC分类号： C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NRx—C(═O)—; —Z1—C(O)—; —Z1—NRx—C(═O)—; —C(═O)—Z1—; —NRx—C(═O)—Z1—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z1—C(═S)—; —Z1—NRx—C(═S)—; —C(═S)—Z1-; NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z 2—NRy—C(=0)—; —NRx—C(=0)-Z2—NRy—C(=0)-; O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(═O)—O—Z2—O—C(═O)—; —NRx—C(═O)—Z2—C(═O)—NRy—; —NRx—C(═O)—Z2—NRy—C(=0)-NRy—; —C(═O)—Z2—; —C(═O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)—NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(═O)—Z2—; —NRx—C(=0)-Z2—NRy; —NRx—C(═O)—Z2—C(═O)—NRy—; —C(═O)—Z2—; —NRx—C(=0)-Z2—NRy—C(=0)—NRy—; —C(═O)—NR—Z2—; —C(═O)—NR—O—Z2—; or —C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents —O—C(═O)—; the R2 O represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

公开(公告)号：US08981094B2

公开(公告)日：2015-03-17

申请号：US12663013

申请日：2008-06-06

申请人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Petr Vladimirivich Davidenko

IPC分类号： C07D211/00 ,  C07D241/04 ,  C07D295/00 ,  C07D401/00 ,  C07D403/00 ,  C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

CPC分类号： C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NRx—C(═O)—; —Z1—C(O)—; —Z1—NRx—C(═O)—; —C(═O)—Z1—; —NRx—C(═O)—Z1—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z1—C(═S)—; —Z1—NRx—C(═S)—; —C(═S)—Z1-; —NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(═O)—O—Z2—O—C(═O)—; —NRx—C(═O)—Z2—C(═O)—NRy—; —NRx—C(═O)—Z2—NRy—C(=0)-NRy—; —C(═O)—Z2—; —C(═O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRX—C(═O)—Z2—; —NRx—C(=0)-Z2—NRy; —NRX—C(═O)—Z2—C(═O)—NRy—; —C(═O)—Z2—; —NRx—C(=0)-Z2—NRy—C(=0)-NRy—; —C(═O)—NRX—Z2—; —C(═O)—NRX—O—Z2—; or —C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents —O—C(═O)—; the R2 represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

公开(公告)号：US08946228B2

公开(公告)日：2015-02-03

申请号：US12663011

申请日：2008-06-06

申请人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

IPC分类号： A61K31/4965 ,  C07D241/04 ,  C07D295/00 ,  A61K31/451 ,  A61K31/495 ,  C07D207/323 ,  C07D211/26 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

CPC分类号： A61K31/4523 ,  A61K31/451 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  C07D207/277 ,  C07D207/323 ,  C07D211/26 ,  C07D211/60 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D295/205 ,  C07D295/21 ,  C07D295/215 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

摘要： The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.

摘要翻译： 本发明涉及式（I）的DGAT抑制剂，包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物，以及制备这些化合物的方法，包含所述化合物的药物组合物 作为所述化合物作为DGAT抑制剂的药物使用。

公开(公告)号：US08835437B2

公开(公告)日：2014-09-16

申请号：US12663009

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Nestor Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

发明人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Nestor Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

IPC分类号： A61K31/496 ,  C07D487/04 ,  C07D513/04 ,  C07D239/42 ,  C07D239/26 ,  A61K31/506 ,  A61K31/454 ,  C07D231/12 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D401/10

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D487/04

摘要： The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p—; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

摘要翻译： 本发明还涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含1或2个N原子的6元芳族杂环，其中所述C3 6-环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 其N-氧化物，其药学上可接受的盐或其溶剂合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

公开(公告)号：US20100216809A1

公开(公告)日：2010-08-26

申请号：US12663009

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

发明人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

IPC分类号： A61K31/506 ,  A61K31/496 ,  A61K31/454 ,  C07D403/10 ,  C07D413/10 ,  C07D513/04 ,  C07D487/04 ,  C07D401/10 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D487/04

摘要： The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

摘要翻译： 本发明还涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含1或2个N原子的6元芳族杂环，其中所述C3 6-环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 其N-氧化物，其药学上可接受的盐或其溶剂合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

公开(公告)号：US07816360B2

公开(公告)日：2010-10-19

申请号：US12341567

申请日：2008-12-22

申请人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Libuse Jaroskova ,  Peter Walter Maria Roevens ,  Louis Jozef Elisabeth Van Der Veken ,  Marcel Viellevoye ,  Joannes Theodorus Maria Linders

发明人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Libuse Jaroskova ,  Peter Walter Maria Roevens ,  Louis Jozef Elisabeth Van Der Veken ,  Marcel Viellevoye ,  Joannes Theodorus Maria Linders

IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D233/74 ,  C07D249/12

CPC分类号： C07D233/54 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

摘要翻译： 本发明涉及用具有apoB分泌/ MTP抑制活性和伴随的降脂活性的某些5-元杂环取代的新的芳基哌啶或哌嗪化合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗高脂血症，肥胖症和II型糖尿病的药物的用途。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

公开(公告)号：US07504400B2

公开(公告)日：2009-03-17

申请号：US10589515

申请日：2005-03-07

申请人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Libuse Jaroskova ,  Peter Walter Maria Roevens ,  Louis Jozef Elisabeth Van Der Veken ,  Marcel Viellevoye ,  Joannes Theodorus Maria Linders

发明人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Libuse Jaroskova ,  Peter Walter Maria Roevens ,  Louis Jozef Elisabeth Van Der Veken ,  Marcel Viellevoye ,  Joannes Theodorus Maria Linders

IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D295/15 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D417/121

CPC分类号： C07D233/54 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper-triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

摘要翻译： 本发明涉及用具有apoB分泌/ MTP抑制活性和伴随的降脂活性的某些5-元杂环取代的新的芳基哌啶或哌嗪化合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗高脂血症，肥胖症和II型糖尿病的药物的用途。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途 。

公开(公告)号：US20100004263A1

公开(公告)日：2010-01-07

申请号：US12341567

申请日：2008-12-22

申请人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Libuse Jaroskova ,  Peter Walter Maria Roevens ,  Louis Jozef Elisabeth Van Der Veken ,  Marcel Viellevoye ,  Joannes Theodorus Maria Linders

发明人： Lieven Meerpoel ,  Leo Jacobus Jozef Backx ,  Libuse Jaroskova ,  Peter Walter Maria Roevens ,  Louis Jozef Elisabeth Van Der Veken ,  Marcel Viellevoye ,  Joannes Theodorus Maria Linders

IPC分类号： A61K31/497 ,  C07D409/02 ,  C07D409/14 ,  C07D411/14 ,  C07D413/04 ,  A61K31/454 ,  A61K31/445 ,  A61P3/10

CPC分类号： C07D233/54 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

摘要翻译： 本发明涉及用具有apoB分泌/ MTP抑制活性和伴随的降脂活性的某些5-元杂环取代的新的芳基哌啶或哌嗪化合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗高脂血症，肥胖症和II型糖尿病的药物的用途。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

公开(公告)号：US08278466B2

公开(公告)日：2012-10-02

申请号：US12989684

申请日：2009-04-27

申请人： Bruno Schoentjes ,  Alain Philippe Poncelet ,  Julien Georges Pierre-Olivier Doyon ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Luc August Laurentius Ver Donck

发明人： Bruno Schoentjes ,  Alain Philippe Poncelet ,  Julien Georges Pierre-Olivier Doyon ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Luc August Laurentius Ver Donck

IPC分类号： C07D313/00 ,  C07C211/00

CPC分类号： C07C215/42 ,  C07C35/52 ,  C07C43/192 ,  C07C215/64 ,  C07C217/08 ,  C07C217/74 ,  C07C2602/12 ,  C07D207/06 ,  C07D213/53 ,  C07D213/65 ,  C07D215/14 ,  C07D239/26 ,  C07D295/092 ,  C07D295/096 ,  C07D295/16 ,  C07D313/08 ,  C07D317/58 ,  C07D405/04 ,  C07D407/04

摘要： The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.

摘要翻译： 本发明涉及包括其任何立体化学异构体形式的式（I）化合物，其中取代基如说明书和权利要求中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是其或其药学上可接受的盐。 要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。 本发明还涉及其药物组合物及其制备方法。

公开(公告)号：US08703973B2

公开(公告)日：2014-04-22

申请号：US13597293

申请日：2012-08-29

申请人： Bruno Schoentjes ,  Alain Philippe Poncelet ,  Julien Georges Pierre-Olivier Doyon ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Luc August Laurentius Ver Donck

发明人： Bruno Schoentjes ,  Alain Philippe Poncelet ,  Julien Georges Pierre-Olivier Doyon ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Luc August Laurentius Ver Donck

IPC分类号： C07D305/00 ,  C07C211/00

CPC分类号： C07C215/42 ,  C07C35/52 ,  C07C43/192 ,  C07C215/64 ,  C07C217/08 ,  C07C217/74 ,  C07C2602/12 ,  C07D207/06 ,  C07D213/53 ,  C07D213/65 ,  C07D215/14 ,  C07D239/26 ,  C07D295/092 ,  C07D295/096 ,  C07D295/16 ,  C07D313/08 ,  C07D317/58 ,  C07D405/04 ,  C07D407/04

摘要： The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than  or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.

摘要翻译： 本发明涉及包括其任何立体化学异构体形式的式（I）化合物，其中取代基如说明书和权利要求中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是其或其药学上可接受的盐。 要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。 本发明还涉及其药物组合物及其制备方法。